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1. 发明授权

US07517902B2 Substituted indazoles, compositions containing the same, and the preparation and use thereof 失效
标题翻译：取代的吲唑，含有它们的组合物及其制备和用途
公开(公告)号：US07517902B2
公开(公告)日：2009-04-14
申请号：US11566382
申请日：2006-12-04
申请人： Frank Halley , Michel Tabart , Hervé Bouchard , Catherine Souaille , Alain Le Brun , Fabrice Viviani , Laurence Gauzy-Lazo , Pascal Desmazeau , Odile Angouillant-Boniface , Bruno Filoche-Romme
发明人： Frank Halley , Michel Tabart , Hervé Bouchard , Catherine Souaille , Alain Le Brun , Fabrice Viviani , Laurence Gauzy-Lazo , Pascal Desmazeau , Odile Angouillant-Boniface , Bruno Filoche-Romme
IPC分类号： A61K31/541 , A61K31/5377 , C07D417/02 , C07D413/02
CPC分类号： C07D231/56 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14
摘要： Disclosed are novel substituted indazole compounds, pharmaceutical compositions comprising such compounds, and methods of treatment comprising such compounds.
摘要翻译：公开了新的取代的吲唑化合物，包含这些化合物的药物组合物和包含这些化合物的治疗方法。

2. 发明申请

US20070161626A1 Substituted Indazoles, Compositions Containing The Same, And The Preparation And Use Thereof 失效
标题翻译：取代的吲唑，含有它的组合物及其制备和使用
公开(公告)号：US20070161626A1
公开(公告)日：2007-07-12
申请号：US11566382
申请日：2006-12-04
申请人： Frank Halley , Michel Tabart , Herve Bouchard , Catherine Souaille , Alain Le Brun , Fabrice Viviani , Laurence Gauzy-Lazo , Pascal Desmazeau , Odile Angouillant-Boniface , Bruno Filoche-Romme
发明人： Frank Halley , Michel Tabart , Herve Bouchard , Catherine Souaille , Alain Le Brun , Fabrice Viviani , Laurence Gauzy-Lazo , Pascal Desmazeau , Odile Angouillant-Boniface , Bruno Filoche-Romme
IPC分类号： A61K31/55 , A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/506 , A61K31/4439 , A61K31/427 , A61K31/422 , A61K31/416 , A61K31/4178 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D231/56 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14
摘要： Disclosed are novel substituted indazole compounds, pharmaceutical compositions comprising such compounds, and methods of treatment comprising such compounds.
摘要翻译：公开了新的取代的吲唑化合物，包含这些化合物的药物组合物和包含这些化合物的治疗方法。

3. 发明申请

US20080125418A1 Benzimidazole derivatives and their use as kdr kinase protein inhibitors 审中-公开
标题翻译：苯并咪唑衍生物及其作为kdr激酶蛋白抑制剂的用途
公开(公告)号：US20080125418A1
公开(公告)日：2008-05-29
申请号：US11943008
申请日：2007-11-20
申请人： Didier Babin , Alain Le Brun , Laurence Gauzy-Lazo , Herve Bouchard
发明人： Didier Babin , Alain Le Brun , Laurence Gauzy-Lazo , Herve Bouchard
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4196 , A61K31/4184 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D487/04 , C07D491/04
摘要： The invention discloses and claims benzimidazole compounds of formula (I): wherein X is C—R2; Y is C—R2 or C—R3; W and Z are each C—R3; R1 is an optionally substituted aryl, heteroaryl or a saturated 5- or 6-membered monocyclic heterocyclic radical or a bicyclic heterocyclic radical; and A5 is H or alkyl; or a stereoisomer, a racemate, an enantiomer or a diastereoisomer of said compound of formula (I) or a pharmaceutically acceptable salt thereof; the use of compounds of formula (I) for the treatment of a disorder of proliferation of blood vessels, uncontrolled angiogenesis, a fibrotic disorder, a disorder of proliferation of mesangial cells, a metabolic disorder, allergy, asthma, thrombosis, a disease of the nervous system, retinopathy, psoriasis, rheumatoid arthritis, diabetes, muscle degeneration, solid tumors and cancers, pharmaceutical compositions comprising a compound of formula (I) and one or more pharmaceutically acceptable adjuvants or diluents and pharmaceutical compositions comprising a compound of formula (I) and one or more. antimitotic agents.
摘要翻译：本发明公开并要求式（I）的苯并咪唑化合物：其中X是C-R2; Y为C-R2或C-R3; W和Z各自为C-R3; R 1是任选取代的芳基，杂芳基或饱和的5-或6-元单环杂环基或双环杂环基; A5是H或烷基; 或所述式（I）化合物的立体异构体，外消旋物，对映异构体或非对映异构体或其药学上可接受的盐; 使用式（I）化合物治疗血管增生障碍，不受控制的血管生成，纤维化病症，肾小球膜细胞增殖障碍，代谢紊乱，过敏，哮喘，血栓形成，疾病神经系统，视网膜病变，银屑病，类风湿性关节炎，糖尿病，肌肉变性，实体瘤和癌症，包含式（I）化合物和一种或多种药学上可接受的佐剂或稀释剂的药物组合物和包含式（I）化合物的药物组合物，和一个或多个。抗有丝分裂剂。

4. 发明申请

US20050009894A1 Benzimidazole derivatives and their use as KDR kinase protein inhibitors 审中-公开
标题翻译：苯并咪唑衍生物及其作为KDR激酶蛋白抑制剂的用途
公开(公告)号：US20050009894A1
公开(公告)日：2005-01-13
申请号：US10828012
申请日：2004-04-20
申请人： Didier Babin , Alain Le Brun , Laurence Gauzy-Lazo , Herve Bouchard
发明人： Didier Babin , Alain Le Brun , Laurence Gauzy-Lazo , Herve Bouchard
IPC分类号： C07D491/056 , A61K31/4184 , A61K31/4188 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61P3/00 , A61P3/10 , A61P7/02 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/04 , C07D491/04 , C07D491/052 , C07D521/00 , A61K31/4196 , C07D471/02
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D487/04 , C07D491/04
摘要： The invention discloses and claims benzimidazole compounds of formula (I): wherein X is C—R2; Y is C—R2 or C—R3; W and Z are each C—R3; R1 is an optionally substituted aryl, heteroaryl or a saturated 5- or 6-membered monocyclic heterocyclic radical or a bicyclic heterocyclic radical; and A5 is H or alkyl; or a stereoisomer, a racemate, an enantiomer or a diastereoisomer of said compound of formula (I) or a pharmaceutically acceptable salt thereof; the use of compounds of formula (I) for the treatment of a disorder of proliferation of blood vessels, uncontrolled angiogenesis, a fibrotic disorder, a disorder of proliferation of mesangial cells, a metabolic disorder, allergy, asthma, thrombosis, a disease of the nervous system, retinopathy, psoriasis, rheumatoid arthritis, diabetes, muscle degeneration, solid tumors and cancers, pharmaceutical compositions comprising a compound of formula (I) and one or more pharmaceutically acceptable adjuvants or diluents and pharmaceutical compositions comprising a compound of formula (I) and one or more. antimitiotic agents.
摘要翻译：本发明公开并要求式（I）的苯并咪唑化合物：其中X是C-R2; Y为C-R2或C-R3; W和Z各自为C-R3; R 1是任选取代的芳基，杂芳基或饱和的5-或6-元单环杂环基或双环杂环基; A5是H或烷基; 或所述式（I）化合物的立体异构体，外消旋物，对映异构体或非对映异构体或其药学上可接受的盐; 使用式（I）化合物治疗血管增生障碍，不受控制的血管生成，纤维化病症，肾小球膜细胞增殖障碍，代谢紊乱，过敏，哮喘，血栓形成，疾病神经系统，视网膜病变，银屑病，类风湿性关节炎，糖尿病，肌肉变性，实体瘤和癌症，包含式（I）化合物和一种或多种药学上可接受的佐剂或稀释剂的药物组合物和包含式（I）化合物的药物组合物，和一个或多个。抗菌剂。

5. 发明授权

US07230007B2 Derivatives of 3-(Guanidinocarbonyl) heterocycle, methods of preparation and intermediates thereof, their use as medicaments, and pharmaceutical compositions therefrom 失效
标题翻译： 3-（胍基羰基）杂环的衍生物，其制备方法及其中间体，其作为药物的用途及其药物组合物
公开(公告)号：US07230007B2
公开(公告)日：2007-06-12
申请号：US10865454
申请日：2004-06-10
申请人： Jean-Christophe Carry , Gilles Doerflinger , Arielle Genevois-Borella , Michel Evers , Alain Le Brun , Jean-Paul Martin , Pascal Desmazeau , Serge Mignani , Heinz-Werner Kleemann
发明人： Jean-Christophe Carry , Gilles Doerflinger , Arielle Genevois-Borella , Michel Evers , Alain Le Brun , Jean-Paul Martin , Pascal Desmazeau , Serge Mignani , Heinz-Werner Kleemann
IPC分类号： A61K31/44 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention discloses and claims compounds of formula I and their pharmaceutically acceptable salts, and methods of using said compounds of formula I, either alone or in combination with other medicaments, as antiarrhythmic medicaments with a cardioprotective component for prophylaxis or treatment of infarction, for the treatment of angina pectoris, and as inhibitors of pathophysiological processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure. Pharmaceutical compositions comprising compounds of formula I or compounds of formula I in combination with one or more other medicaments and processes for the preparation of compounds of formula I are also disclosed and claimed.
摘要翻译：本发明公开并要求式I化合物及其药学上可接受的盐，以及使用所述式I化合物单独或与其它药物组合的抗心律失常药物与预防或治疗梗死的心脏保护组分的方法，用于心绞痛的治疗以及与局部缺血诱导的损伤发展相关的病理生理过程的抑制剂，特别是引发缺血诱导的心律失常和心力衰竭。包含式I化合物或式I化合物与一种或多种其它药物组合的药物组合物和式I化合物的制备方法也被公开并要求保护。

6. 发明申请

US20050014758A1 Derivatives of 3-(guanidinocarbonyl) heterocycle, methods of preparation and intermediates thereof, their use as medicaments, and pharmaceutical compositions therefrom 失效
标题翻译： 3-（胍基羰基）杂环的衍生物，其制备方法及其中间体，它们作为药物的用途及其药物组合物
公开(公告)号：US20050014758A1
公开(公告)日：2005-01-20
申请号：US10865454
申请日：2004-06-10
申请人： Jean-Christophe Carry , Gilles Doerflinger , Arielle Genevois-Borella , Michel Evers , Alain Le Brun , Jean-Paul Martin , Pascal Desmazeau , Serge Mignani , Heinz-Werner Kleemann
发明人： Jean-Christophe Carry , Gilles Doerflinger , Arielle Genevois-Borella , Michel Evers , Alain Le Brun , Jean-Paul Martin , Pascal Desmazeau , Serge Mignani , Heinz-Werner Kleemann
IPC分类号： C07D471/04 , C07D471/02 , A61K31/4745 , A61K31/503 , A61K31/519 , C07D487/02
CPC分类号： C07D471/04
摘要： The present invention discloses and claims compounds of formula I and their pharmaceutically acceptable salts, and methods of using said compounds of formula I, either alone or in combination with other medicaments, as antiarrhythmic medicaments with a cardioprotective component for prophylaxis or treatment of infarction, for the treatment of angina pectoris, and as inhibitors of pathophysiological processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure. Pharmaceutical compositions comprising compounds of formula I or compounds of formula I in combination with one or more other medicaments and processes for the preparation of compounds of formula I are also disclosed and claimed.
摘要翻译：本发明公开并要求式I化合物及其药学上可接受的盐，以及使用所述式I化合物单独或与其它药物组合的抗心律失常药物与预防或治疗梗死的心脏保护组分的方法，用于心绞痛的治疗以及与局部缺血诱导的损伤发展相关的病理生理过程的抑制剂，特别是引发缺血诱导的心律失常和心力衰竭。包含式I化合物或式I化合物与一种或多种其它药物组合的药物组合物和式I化合物的制备方法也被公开并要求保护。

7. 发明申请

US20050014765A1 Aryl-heteroaromatic products, compositions comprising them and use 审中-公开
标题翻译：芳基杂芳族产物，包含它们的组合物和用途
公开(公告)号：US20050014765A1
公开(公告)日：2005-01-20
申请号：US10859740
申请日：2004-06-03
申请人： Patrick Mailliet , Alain Le Brun , Fabienne Thompson , Gilles Tiraboschi
发明人： Patrick Mailliet , Alain Le Brun , Fabienne Thompson , Gilles Tiraboschi
IPC分类号： C07D207/34 , C07D233/90 , C07D263/34 , C07D277/56 , C07D307/68 , C07D333/38 , C07D401/06 , C07D401/12 , C07D417/06 , A61K31/496 , A61K31/4439 , C07D413/02
CPC分类号： C07D263/34 , C07D207/34 , C07D233/90 , C07D277/56 , C07D307/68 , C07D333/38 , C07D401/06 , C07D401/12 , C07D417/06
摘要： Aryl-heteroaromatic products, compositions comprising them and use. The present invention relates to novel chemical compounds, particularly to novel aryl-heteroaromatic products, to compositions comprising them, and to their use as medicaments, in particular in oncology.
摘要翻译：芳基杂芳族产物，包含它们的组合物和用途。本发明涉及新颖的化合物，特别是新颖的芳基杂芳族产物，包含它们的组合物，以及它们作为药物，特别是在肿瘤学中的用途。

8. 发明授权

US5750567A Farnesyl transferase inhibitors, preparation thereof and pharmaceutical compositions containing same 失效
标题翻译：法呢基转移酶抑制剂，其制备方法和含有其的药物组合物
公开(公告)号：US5750567A
公开(公告)日：1998-05-12
申请号：US875005
申请日：1997-07-15
申请人： Bernard Baudoin , Christopher Burns , Alain Commercon , Alain Le Brun
发明人： Bernard Baudoin , Christopher Burns , Alain Commercon , Alain Le Brun
IPC分类号： A61K31/195 , A61K31/215 , A61P35/00 , A61P43/00 , C07C323/25 , C07C323/59 , A61K31/21
CPC分类号： C07C323/25 , C07C323/59
摘要： Novel farnesyl transferase inhibitors of general formula (I) ##STR1## preparation thereof and pharmaceutical compositions containing same. In general formula (I), R.sub.1 is Y--S--A.sub.1 -- (where Y is a hydrogen atom, an amino acid residue, a fatty acid residue, or an alkyl or alkoxycarbonyl radical, and A.sub.1 is a C.sub.1-4 alkylene radical optionally .alpha.-substituted in the >C(X.sub.1) (Y.sub.1,) grouping by an amino, alkylamino, alkanoylamino or alkoxycarbonylamino radical wherein the alkyl or alkanoyl portion contains 1-6 carbon atoms; each of X.sub.1 and Y.sub.1 is a hydrogen atom or X.sub.1 and Y.sub.1, taken toether with the carbon atom to which they are attached, form a >C.dbd.O grouping; R'.sub.1 is hydrogen or a C.sub.1-6 alkyl radical; X is an oxygen or sulphur atom; R.sub.2 is a C.sub.1-6 alkyl, alkenyl or alkynyl radical optionally substituted by hydroxy, alkoxy, mercapto, alkylthio, alkylsulphinyl or alkylsulphonyl.
摘要翻译： PCT No.PCT / FR96 / 00067 Sec。 371日期1997年7月15日 102（e）日期1997年7月15日PCT 1996年1月16日PCT PCT。公开号WO96 / 22278 日本1996年7月25日通式（I）的新型法呢基转移酶抑制剂（I）其制备方法和含有其的药物组合物。在通式（I）中，R 1为YS-A1-（其中Y为氢原子，氨基酸残基，脂肪酸残基或烷基或烷氧羰基，A1为C1-4亚烷基，在其中烷基或烷酰基部分含有1-6个碳原子的氨基，烷基氨基，烷酰基氨基或烷氧基羰基氨基的基团中被取代> C（X1）（Y1）中的每一个，X1和Y1各自为氢原子或X1和Y1，与其连接的碳原子一起形成C = O基团; R'1是氢或C1-6烷基; X是氧或硫原子; R2是C1-6烷基，烯基或任选被羟基，烷氧基，巯基，烷硫基，烷基亚磺酰基或烷基磺酰基取代的炔基。

9. 发明授权

US5936097A 4,9-ethano-benzo(F)isoindole derivatives as farnesyl transferase inhibitors 失效
标题翻译： 4,9-乙 - 苯并（F）异吲哚衍生物作为法呢基转移酶抑制剂
公开(公告)号：US5936097A
公开(公告)日：1999-08-10
申请号：US981840
申请日：1998-07-23
申请人： Alain Commer.cedilla.on , Alain Le Brun , Patrick Mailliet , Jean-Fran.cedilla.ois Peyronel , Fabienne Sounigo-Thompson , Alain Truchon , Martine Zucco
发明人： Alain Commer.cedilla.on , Alain Le Brun , Patrick Mailliet , Jean-Fran.cedilla.ois Peyronel , Fabienne Sounigo-Thompson , Alain Truchon , Martine Zucco
IPC分类号： C07D409/12 , A61K31/00 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/425 , A61K31/427 , A61P35/00 , A61P43/00 , C07D209/58 , C07D209/72 , C07D277/22 , C07D417/12 , C07F9/572 , C07D209/62 , C07D209/12 , C07D307/36
CPC分类号： C07D209/72 , C07F9/5728
摘要： Novel products of formula (I): ##STR1## preparation thereof and pharmaceutical compositions containing said products are disclosed. In formula (I), R is a group of formula --(CH.sub.2).sub.m --X.sub.1 --(CH.sub.2).sub.n --Z, where X.sub.1 is a simple bond or O or S, n is 0 or 1 and n is 0, 1 or 2, the CH.sub.2 groups being optionally substituted by carboxy, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, amino, alkylamino or dialkylamino, and Z is carboxy, COOR.sub.4, where R.sub.4 is alkyl, or CON(R.sub.5)(R.sub.6), where R.sub.5 hydrogen or alkyl and R.sub.6 is hydrogen or optionally substituted alkyl, or else R.sub.5 is hydrogen or alkyl and R.sub.6 is hydroxy, optionally substituted alkoxy or amino, or PO(OR.sub.7).sub.2, where R.sub.7 is hydrogen or alkyl; or a group --NH--CO--T where T is hydrogen or optionally substituted alkyl; or else a group (a); R.sub.1 and R.sub.2 are hydrogen or halogen or optionally substituted alkyloxy or alkyl, or else R.sub.1 and R.sub.2 in the ortho positions form a heterocyclic ring containing 1 or 2 optionally substituted hereoatoms, or R.sub.1 is hydrogen or halogen or optionally substituted alkyloxy or alkyl, and R.sub.2 is thioalkyl; R.sub.3 is hydrogen or halogen or alkyl alkenyl, alkyloxy, alkylthio, carboxy or alkyloxycarbonyl; X is O or S or --NH--, --CO--,methylene, ethylene, alkylidene or 1,1-cycloalkyl; and Y is O or S. The novel products of formula (I) are farnesyl transferase inhibitors having remarkable antitumoral and antineoplastic properties.
摘要翻译： PCT No.PCT / FR96 / 01062 Sec。 371日期：1998年7月23日 102（e）1998年7月23日PCT PCT 1996年7月8日PCT公布。出版物WO97 / 03050 日期1997年1月30日公开了式（I）的新产物：其制备方法和含有所述产物的药物组合物。在式（I）中，R是式 - （CH2）m-X1-（CH2）nZ的基团，其中X1是简单键或O或S，n是0或1，n是0,1或2， CH 2基任选被羧基，烷氧基羰基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，氨基，烷基氨基或二烷基氨基取代，Z是羧基，COOR 4，其中R 4是烷基或CON（R 5）（R 6） R 6是氢或任选取代的烷基，或者R 5是氢或烷基，R 6是羟基，任选取代的烷氧基或氨基或PO（OR 7）2，其中R 7是氢或烷基; 或基团-NH-CO-T，其中T是氢或任选取代的烷基; 或者一组（a）; R1和R2是氢或卤素或任选取代的烷氧基或烷基，或者邻位中的R1和R2形成含有1或2个任选取代的原子的杂环，或者R 1是氢或卤素或任选取代的烷氧基或烷基，R 2 是硫代烷基; R3是氢或卤素或烷基烯基，烷氧基，烷硫基，羧基或烷氧基羰基; X是O或S或-NH-，-CO-，亚甲基，亚乙基，亚烷基或1,1-环烷基; 并且Y是O或S.式（I）的新产物是具有显着的抗肿瘤和抗肿瘤性质的法呢基转移酶抑制剂。

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